CO2018000793A2 - Adduct of (2e) -but-2-enedioic acid and- 3- (2 - {[4- (trifluoromethoxy) phenyl] amino} -1 - [(1r, 5r) -3,3,5-trimethylcyclohexyl] - acid 1h benzimidazol-5-yl) propanoic (1: 4) as inhibitor of the mutated isocitrate dehydrogenase idh1 r132h, methods for its preparation and compositions that comprise it - Google Patents

Adduct of (2e) -but-2-enedioic acid and- 3- (2 - {[4- (trifluoromethoxy) phenyl] amino} -1 - [(1r, 5r) -3,3,5-trimethylcyclohexyl] - acid 1h benzimidazol-5-yl) propanoic (1: 4) as inhibitor of the mutated isocitrate dehydrogenase idh1 r132h, methods for its preparation and compositions that comprise it

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Publication number
CO2018000793A2
CO2018000793A2 CONC2018/0000793A CO2018000793A CO2018000793A2 CO 2018000793 A2 CO2018000793 A2 CO 2018000793A2 CO 2018000793 A CO2018000793 A CO 2018000793A CO 2018000793 A2 CO2018000793 A2 CO 2018000793A2
Authority
CO
Colombia
Prior art keywords
acid
adduct
trimethylcyclohexyl
benzimidazol
propanoic
Prior art date
Application number
CONC2018/0000793A
Other languages
Spanish (es)
Inventor
Heiko Schirmer
Original Assignee
Bayer Pharma AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of CO2018000793A2 publication Critical patent/CO2018000793A2/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Abstract

La presente invención se refiere al aducto del ácido (2E)-But-2-enedioico y ácido- 3-(2-{[4-(trifluorometoxi)fenil]amino}-1-[(1R,5R)-3,3,5-trimetilciclohexil]-1H benzimidazol-5-il)propanoico (1:4) como inhibidor de la isocitrato deshidrogenasa mutada IDH1 R132H, a métodos para preparar este aducto y a composiciones que comprenden este aducto.”The present invention relates to the adduct of (2E) -But-2-enedioic acid and acid- 3- (2 - {[4- (trifluoromethoxy) phenyl] amino} -1 - [(1R, 5R) -3,3 , 5-trimethylcyclohexyl] -1H benzimidazol-5-yl) propanoic (1: 4) as inhibitor of the mutated isocitrate dehydrogenase IDH1 R132H, to methods for preparing this adduct and to compositions comprising this adduct.

CONC2018/0000793A 2015-07-27 2018-01-26 Adduct of (2e) -but-2-enedioic acid and- 3- (2 - {[4- (trifluoromethoxy) phenyl] amino} -1 - [(1r, 5r) -3,3,5-trimethylcyclohexyl] - acid 1h benzimidazol-5-yl) propanoic (1: 4) as inhibitor of the mutated isocitrate dehydrogenase idh1 r132h, methods for its preparation and compositions that comprise it CO2018000793A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP15178419 2015-07-27
PCT/EP2016/067477 WO2017016992A1 (en) 2015-07-27 2016-07-22 Inhibitor of the mutated isocitrate dehydrogenase idh1 r132h

Publications (1)

Publication Number Publication Date
CO2018000793A2 true CO2018000793A2 (en) 2018-05-10

Family

ID=53758092

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2018/0000793A CO2018000793A2 (en) 2015-07-27 2018-01-26 Adduct of (2e) -but-2-enedioic acid and- 3- (2 - {[4- (trifluoromethoxy) phenyl] amino} -1 - [(1r, 5r) -3,3,5-trimethylcyclohexyl] - acid 1h benzimidazol-5-yl) propanoic (1: 4) as inhibitor of the mutated isocitrate dehydrogenase idh1 r132h, methods for its preparation and compositions that comprise it

Country Status (26)

Country Link
US (1) US10344004B2 (en)
EP (1) EP3328837B1 (en)
JP (1) JP6804516B2 (en)
KR (1) KR20180030789A (en)
CN (1) CN107810181B (en)
AR (1) AR105493A1 (en)
AU (1) AU2016300980B2 (en)
BR (1) BR112018001534A2 (en)
CA (1) CA2993473A1 (en)
CL (1) CL2018000249A1 (en)
CO (1) CO2018000793A2 (en)
CR (1) CR20180053A (en)
CU (1) CU20180014A7 (en)
DO (1) DOP2018000027A (en)
EA (1) EA201890386A1 (en)
EC (1) ECSP18006465A (en)
ES (1) ES2860693T3 (en)
HK (1) HK1252449A1 (en)
IL (1) IL256024A (en)
MX (1) MX2018001205A (en)
NI (1) NI201800014A (en)
PE (1) PE20181038A1 (en)
SV (1) SV2018005621A (en)
TN (1) TN2018000038A1 (en)
TW (1) TW201708193A (en)
WO (1) WO2017016992A1 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3105210B1 (en) 2014-02-11 2019-01-30 Bayer Pharma Aktiengesellschaft Benzimidazol-2-amines as midh1 inhibitors
EA031655B1 (en) 2014-02-11 2019-02-28 Байер Фарма Акциенгезельшафт BENZIMIDAZOL-2-AMINES AS mIDH1 INHIBITORS
EP3209660B1 (en) 2014-10-23 2020-06-17 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts 1-cyclohexyl-2-phenylaminobenzimidazoles as midh1 inhibitors for the treatment of tumors
EP3303302B1 (en) 2015-06-08 2019-03-20 Bayer Pharma Aktiengesellschaft N-menthylbenzimidazoles as midh1 inhibitors
US10179123B2 (en) 2015-07-07 2019-01-15 Bayer Pharma Aktiengesellschaft 2-aryl- and 2-arylalkyl-benzimidazoles as mIDH1 inhibitors
JP6824954B2 (en) 2015-07-16 2021-02-03 ドイチェス クレープスフォルシュングスツェントルム シュティフトゥング デス エッフェントリッヒェン レヒツ 5-Hydroxyalkylbenzimidazole as an mIDH1 inhibitor
EP3121166A1 (en) 2015-07-21 2017-01-25 Bayer Pharma Aktiengesellschaft Fused imidazoles as midh1 inhibitors
TW201718513A (en) 2015-07-27 2017-06-01 拜耳製藥公司 Method for preparing substituted 3-(2-anilino-1-cyclohexyl-1H-benzimidazol-5-yl)propanoic acid derivatives
WO2019015672A1 (en) * 2017-07-21 2019-01-24 南京明德新药研发股份有限公司 Pyridoimidazole compound and use thereof
CA3070878A1 (en) * 2017-08-01 2019-02-07 Deutsches Krebsforschungszentrum Combination of midh1 inhibitors and dna hypomethylating agents (hma)
CN108948205B (en) * 2018-07-13 2021-09-28 北京金岱生物科技有限公司 anti-IDH 1R132H monoclonal antibody and application thereof
TWI760017B (en) * 2019-12-23 2022-04-01 大陸商昆藥集團股份有限公司 Salt form, crystalline form of idh1 mutant inhibitor and preparation method thereof
CN116348145A (en) 2020-07-21 2023-06-27 第一三共株式会社 Combination of temozolomide and mutant IDH1 enzyme inhibitor

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010151441A1 (en) * 2009-06-23 2010-12-29 Translational Genomics Research Institute Benzamide derivatives
EP2643314B1 (en) * 2010-11-25 2016-07-13 ratiopharm GmbH Novel salts and polymorphic forms of afatinib
CN103958506B (en) * 2011-09-27 2017-02-22 诺华股份有限公司 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
EP3105210B1 (en) 2014-02-11 2019-01-30 Bayer Pharma Aktiengesellschaft Benzimidazol-2-amines as midh1 inhibitors
EA031655B1 (en) * 2014-02-11 2019-02-28 Байер Фарма Акциенгезельшафт BENZIMIDAZOL-2-AMINES AS mIDH1 INHIBITORS
CN107108522B (en) * 2014-10-23 2020-12-01 德国癌症研究中心 Benzimidazol-2-amines as mIDH1 inhibitors
EP3209660B1 (en) * 2014-10-23 2020-06-17 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts 1-cyclohexyl-2-phenylaminobenzimidazoles as midh1 inhibitors for the treatment of tumors
EP3303302B1 (en) 2015-06-08 2019-03-20 Bayer Pharma Aktiengesellschaft N-menthylbenzimidazoles as midh1 inhibitors
US10179123B2 (en) 2015-07-07 2019-01-15 Bayer Pharma Aktiengesellschaft 2-aryl- and 2-arylalkyl-benzimidazoles as mIDH1 inhibitors
JP6824954B2 (en) * 2015-07-16 2021-02-03 ドイチェス クレープスフォルシュングスツェントルム シュティフトゥング デス エッフェントリッヒェン レヒツ 5-Hydroxyalkylbenzimidazole as an mIDH1 inhibitor
EP3121166A1 (en) 2015-07-21 2017-01-25 Bayer Pharma Aktiengesellschaft Fused imidazoles as midh1 inhibitors
TW201718513A (en) * 2015-07-27 2017-06-01 拜耳製藥公司 Method for preparing substituted 3-(2-anilino-1-cyclohexyl-1H-benzimidazol-5-yl)propanoic acid derivatives

Also Published As

Publication number Publication date
CA2993473A1 (en) 2017-02-02
AU2016300980B2 (en) 2020-12-24
EP3328837B1 (en) 2021-01-06
TW201708193A (en) 2017-03-01
JP2018521095A (en) 2018-08-02
MX2018001205A (en) 2018-04-24
PE20181038A1 (en) 2018-07-03
BR112018001534A2 (en) 2018-09-11
ECSP18006465A (en) 2018-04-30
CN107810181B (en) 2021-06-22
TN2018000038A1 (en) 2019-07-08
IL256024A (en) 2018-01-31
JP6804516B2 (en) 2020-12-23
EP3328837A1 (en) 2018-06-06
ES2860693T3 (en) 2021-10-05
CL2018000249A1 (en) 2018-07-06
HK1252449A1 (en) 2019-05-24
CU20180014A7 (en) 2018-06-05
CN107810181A (en) 2018-03-16
US10344004B2 (en) 2019-07-09
SV2018005621A (en) 2018-12-05
WO2017016992A1 (en) 2017-02-02
AU2016300980A1 (en) 2017-12-21
NI201800014A (en) 2018-09-06
AR105493A1 (en) 2017-10-11
KR20180030789A (en) 2018-03-26
US20180222870A1 (en) 2018-08-09
DOP2018000027A (en) 2018-02-28
EA201890386A1 (en) 2018-08-31
CR20180053A (en) 2018-03-20

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